You have reached the HIVandHepatitis.com legacy site. Please visit our new site at hivandhepatitis.com

Entecavir (Baraclude)

Prescribing Information
Entecavir (Baraclude): An Overview
Important Safety Information

Articles on Entecavir (Baraclude)

Entecavir Effective for Hepatitis B Patients with Liver Cancer
6-28-2011

Prolonged Entecavir for Slow Responders
6-3-2011

Switch to Lamivudine Not as Effective as Staying on Entecavir
5-6-2011

Entecavir Beats Adefovir for Hepatitis B Treatment
3-29-2011

Entecavir Approved in Europe for Hepatitis B Patients with Decompensated Liver Diseases
3-11-2011

Tenofovir and Entecavir Are Safe and Effective in Hepatitis B Patients with Decompensated Cirrhosis
1-18-2011

Bristol-Myers Squibb Enhances Co-pay Assistance Program for Entecavir (Baraclude) for Hepatitis B
11/15/2010

Entecavir (Baraclude) Continues to Suppress HBV for 5 Years in Asian Patients
11/09/2010

Efficacy and Safety of Entecavir in Nucleos(t)ide Naïve Asians With HBeAg-Positive and -Negative Chronic Hepatitis B: Results from Studies ETV-022/027
11/09/2010

Long-term Entecavir Treatment for Up to 5 Years in Asians With HBeAg-positive Chronic Hepatitis B: Results From ETV-022 and -901
11/09/2010

Meta-analysis Finds Tenofovir and Entecavir Are Most Effective Antiviral Drugs for Chronic Hepatitis B
8-24-2010


How Long Do Chronic Hepatitis B Patients Need to be Treated to Sustain HBeAg Seroconversion?
6-25-2010

Entecavir (Baraclude) Works Well in Patients with Adefovir-resistant Hepatitis B, but Lamivudine Resistance Compromises Efficacy
4-02-2010

Hepatitis B Surface Antigen Loss during Treatment with Entecavir (Baraclude) or Lamivudine (Epivir-HBV)
2-12-2010

Entecavir (Baraclude) Improves Liver Function in Chronic Hepatitis B Patients with Decompensated Cirrhosis
2-09-2010

Long-term Entecavir (Baraclude) Produces Sustained Viral Suppression with Little Resistance in HBeAg Positive Chronic Hepatitis B Patients
1-26-2010

Chronic Hepatitis B Patients with Liver Cirrhosis Are at Risk for Lactic Acidosis after Starting Entecavir (Baraclude)
1-19-2010

Efficacy and Safety of Entecavir Versus Adefovir in Chronic Hepatitis B Patients with Evidence of Hepatic Decompensation
11-03-2009

Loss of HBsAg in Nucleoside-Naïve HBeAg(+) Chronic Hepatitis B Patients Following Treatment with Entecavir or Lamivudine: Evaluation of HBV Genotypes
11-01-2009

AASLD Issues Updated Practice Guidelines for Management of Chronic Hepatitis B
9-22-2009

Entecavir (ETV) Therapy in Chronic Hepatitis B Patients Previously Treated with Adefovir (ADV) with Incomplete Response On-Treatment or Relapse Off-Treatment
6/05/09

Long-Term Histological Improvement with Entecavir (ETV) Therapy in Patients with Chronic Hepatitis B (CHB) from Japanese and Worldwide Development Programs
6/05/09

Entecavir Maintains a High Genetic Barrier to HBV Resistance Through 6 Years in Na´ve Patients
6/05/09

Regression of Fibrosis/Cirrhosis with Long-Term Entecavir Therapy in Chronic Hepatitis B (CHB) Patients with Baseline Bridging Fibrosis or Cirrhosis: Results from Studies ETV-022, -027 and -901
6/05/09

Should Entecavir (Baraclude) and Tenofovir (Viread) Be First-line Treatment for Chronic Hepatitis B?
6/05/09

Chronic Hepatitis B Patients Who Had Incomplete Response or Relapse on Adefovir (Hepsera) Respond Well to Entecavir (Baraclude)

5/01/09

Entecavir (Baraclude) Produces Greater Early HBV DNA Suppression than Adefovir (Hepsera) in Chronic Hepatitis B Patients
3/17/09


HBV Relapse after 48 Weeks of Entecavir (Baraclude) Suggests Need for Continuous Therapy
2/24/2009


Japanese Study Finds Entecavir (Baraclude) Is Effective and Well-tolerated in Treatment-naive Chronic Hepatitis B Patients
2/10/2009



Entecavir (Baraclude): An Overview
Brand Name: Baraclude
Drug Class: Nucleoside analogue reverse transcriptase inhibitor

Introduction

Entecavir (Baraclude) is a nucleoside analogue drug that has selective anti-hepatitis B virus (HBV) activity. The US Food and Drug Administration (FDA) approved entecavir, an orally administered drug, on March 30, 2005 for the treatment of chronic hepatitis B infection in adults.

The FDA also approved entecavir for the treatment of chronic hepatitis B in adults with HIV coinfection. However, entecavir is not active against HIV and is not approved for that purpose.

Entecavir is indicated for treatment of chronic hepatitis B infection in adults with active viral replication and who show elevations in ALT or AST (aminotransferases) or histologically active disease (fibrosis or cirrhosis).

Baraclude does not cure HBV or stop the spread of HBV to others. People should not take Baraclude if they are allergic to it or any of its ingredients. Baraclude has not been studied in children and is not recommended for anyone less than 16 years of age.

FDA approval of entecavir was based on the results of three studies that compared entecavir to lamivudine (Epivir-HBV), another nucleoside analog that is FDA-approved for treatment of chronic hepatitis B. In all 3 studies, patients treated with entecavir showed significant improvement in the liver inflammation caused by HBV and an improvement in the degree of liver fibrosis (scarring). In addition, a higher percentage of patients treated with e ntecavir showed significant overall improvement compared to lamivudine.

Dosing

The recommended dosage of entecavir is a single 0.5 mg tablet once-daily for chronic hepatitis B patients beginning treatment for the first time (nucleoside-na´ve patients), and a single 1 mg tablet once-daily for patients experiencing resistance to lamivudine.

Entecavir comes in tablet and oral suspension forms and is taken by mouth without food. The tablets are film-coated, triangular-shaped and contain 0.5 or 1.0 mg entecavir. The oral solution contains 0.05 mg/ml entecavir in a 260 ml bottle.

Entecavir should be taken 2 hours after a meal and 2 hours before the next meal. Based on the pharmacokinetic profile of entecavir after oral dosing, the estimated apparent volume of distribution is in excess of total body water, suggesting that entecavir is extensively distributed into tissues.

Pharmacology

Pregnancy

Entecavir is in FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Reproduction studies have been performed in rats and rabbits at orally administered doses of 200 and 16 mg/kg/day and showed no embryo-toxicity or maternal toxicity in rat and rabbit at doses producing systemic exposures approximately 28 and 212 times those achieved at the highest recommended dose of 1 mg/day in humans.

In rats, maternal toxicity, embryo-fetal toxicity (resorptions), lower fetal body weights, tail and vertebral malformations, reduced ossification (vertebrae, sternebrae, and phalanges), and extra lumbar vertebrae and ribs were observed at exposures 3,100 times those in humans.

Because animal reproduction studies are not always predictive of human response, entecavir should be used during pregnancy only if clearly needed and after careful consideration of the risks and benefits. To monitor fetal outcomes of pregnant women exposed to entecavir, an Antiretroviral Pregnancy Registry has been established. Healthcare providers are encouraged to register patients online at http://www.APRegistry.com or by calling 1-800-258-4263.

Food and Drug Interactions

Food Interactions

Oral administration of entecavir 0.5 mg with a standard high-fat meal (945 kcal, 54.6 g fat) or a light meal (379 kcal, 8.2 g fat) resulted in delayed absorption (1.0 to 1.5 hour fed vs. 0.75 hours fasted), a decrease in Cmax of 44% to 46%, and a decrease in AUC of 18% to 20%. For this reason, and for best results, it is recommended to take entecavir 2 hours after a meal and 2 hours before the next meal.

The pharmacokinetics of entecavir following a single 1 mg dose were studied in patients without chronic hepatitis B infection with selected degrees of renal impairment. Dosage adjustment is recommended for patients with a creatinine clearance of less than 50 ml/min, including patients on hemodialysis or continuous ambulatory peritoneal dialysis (CAPD). Entecavir should be administered after hemodialysis. CAPD removed approximately 0.3% of the dose over 7 days.

Drug Interactions

Coadministration of the HIV nucleoside/tide analogues with entecavir does not appear to reduce the antiviral efficacy of entecavir against HBV or of any of these agents against HBV. In HBV combination assays in vitro, (Ziagen), (Videx), (Epivir-HBV), (Zerit), (Viread), and (Retrovir) were not antagonistic to the anti-HBV activity of entecavir over a wide range of concentrations. In HIV antiviral assays, entecavir was not antagonistic to the in vitro anti-HIV activity of these NRTIs at greater than 4 times the Cmax of entecavir.

Cross resistance has been observed among HBV nucleoside analogues. In cell-based assays entecavir had 8- to 30-fold less inhibition of replication of HBV that contained lamivudine resistance mutations rtL180M and rtM204V/I than of wild-type vius.


Important Safety Information

Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues alone or in combination with antiretrovirals.

Severe acute exacerbations of hepatitis B have been reported in patients who have discontinued anti-hepatitis B therapy, including BARACLUDE. Hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in patients who discontinue anti-hepatitis B therapy. If appropriate, initiation of anti-hepatitis B therapy may be warranted.

Limited clinical experience suggests there is a potential for the development of resistance to HIV (human immunodeficiency virus) nucleoside reverse transcriptase inhibitors if BARACLUDE is used to treat chronic hepatitis B virus infection in patients with HIV infection that is not being treated. Therapy with BARACLUDE is not recommended for HIV/HBV co-infected patients who are not also receiving highly active antiretroviral therapy (HAART). Before initiating BARACLUDE therapy, HIV antibody testing should be offered to all patients.

BARACLUDE has not been studied as a treatment for HIV infection and is not recommended for this use.

Dosage adjustment of BARACLUDE is recommended for patients with a creatinine clearance <50 mL/min, patients with age-related decreases in renal function, and those on hemodialysis or continuous ambulatory peritoneal dialysis (CAPD).

Since entecavir is primarily eliminated by the kidneys, coadministration of BARACLUDE with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of either entecavir or the coadministered drug.

The safety and efficacy of BARACLUDE in liver transplant recipients are unknown. Renal function must be carefully monitored both before and during treatment with BARACLUDE in a liver transplant recipient who has received or is receiving an immunosuppressant that may affect renal function, such as cyclosporine or tacrolimus.

Patients should be advised that treatment with BARACLUDE has not been shown to reduce the risk of transmission of HBV to others through sexual contact or blood contamination.

There are no adequate and well-controlled studies of BARACLUDE administered to pregnant women. BARACLUDE should be used during pregnancy only if clearly needed and after careful consideration of the risks and benefits. There are no studies on the effect of BARACLUDE on transmission of HBV from mother to infant. Therefore, appropriate interventions should be used to prevent neonatal acquisition of HBV. Women should be instructed not to breast-feed if they are taking BARACLUDE.

Safety and effectiveness of BARACLUDE in pediatric patients below the age of 16 years have not been established.

The most common adverse events of moderate to severe intensity among patients treated with BARACLUDE in clinical trials included: headache (4%), fatigue (3%), diarrhea (1%), and dyspepsia (1%).

The recommended dose of BARACLUDE is 0.5 mg once daily in nucleoside-naïve adults, and 1 mg once daily in lamivudine-refractory adults. BARACLUDE should be administered on an empty stomach (at least 2 hours after a meal and at least 2 hours before the next meal). The optimal duration of treatment with BARACLUDE for patients with chronic hepatitis B infection and the relationship between treatment and long-term outcomes such as cirrhosis and hepatocellular carcinoma are unknown.

 

 

 

 

 

 

 

 

 



 

 

 

 

 

 

 

 

 

 

 

 


 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 



 Google Custom Search
FDA-approved Therapies for Chronic HBV Infection
Baraclude  (entecavir)
Epivir-HBV
  (lamivudine; 3TC)
Hepsera
  (adefovir dipivoxil)
Intron A  (interferon alfa-2b)
Pegasys  (peginterferon alfa-2a)
Viread  (tenofovir)
Tyzeka   (telbivudine)

Experimental Treatments

HBV Articles by Topic

Cirrhosis
Fibrosis
Hepatocellular Carcinoma
Liver Transplantation

Steatosis
Children / Infants / Women
Hepatitis B Clinical Trials
Experimental Treatments
FAQs About Hepatitis
Genotypes
Guidelines
Tests for HBV
Vaccines for HBV